目的研究三七素的理化性质及渗透促进剂对三七素体外透皮性能的影响。方法采用摇瓶法测定三七素的表观溶解度及油水分配系数;采用Franz扩散池法,以小鼠皮和猪皮为模型皮肤,采用HPLC法测定三七素,评价最佳促渗剂。结果三七素水溶性强,lg P值低,三七素在皮肤上体外释放符合Higuchi方程;在小鼠皮上的渗透效果比猪皮好;通过对促渗剂种类和用量的筛选,发现5%N-甲基-2-吡咯烷酮(NMP)促渗效果最好。结论三七素具有一定的经皮吸收能力,其经皮吸收与药物在皮肤中的扩散速率有关,5%NMP显著增加三七素经皮渗透速率。
Objective To evaluate the percutaneous absorption properties of dencichine. Methods Shaking flask method was used to determine the apparent solubility and oil-water partition coefficient of dencichine. The Franz diffusion cell method was adopted and skin of mice and pig was used as the model skin. The content of dencichine and optimized penetration enhancer were determined using HPLC. Results Dencichine is water soluble with a low lg P value. Dencichine showed a better penetrability in mice skin than in pig skin. The permeation profiles of dencichine can be fitted well by Higuchi model. The significant percutaneous absorption for dencichine is 5% NMP. Conclusion Dencichine shows the certain perctaneous absorption ability. And the skin permeation profiles are related with the diffusion rate of the drug in skin. The permeability rate could be promoted by 5% NMP.